Nolvadex

Really, if the truth were known, this was the very first compound used as an “ancillary” medication by steroid-using athletes. Dan Duchaine had first speculated that it could possibly be used by bodybuilders to halt the development of gynocomastia (breast tissue in males), because it was used to stop breast tumors in women. He was, as usual, correct. Since then, Nolvadex has become the most widely used medication in the world for men on a steroids looking to avoid gyno.

Nolvadex is a SERM or Selective Estrogen Receptor Modulator. The “selective” part means that it acts as an estrogen agonist in some tissues and as an estrogen antagonist in others. The “Estrogen Receptor Modulator” part means that it acts on the Estrogen Receptor (called the "ER" but having nothing to do with George Clooney or Anthony Edwards).

The estrogen receptor's ligand binding domain is just of a number of amino acid sequences "folded" into a series of helixes, which have the ability to change conformation. Different stimuli (such as Nolvadex) are well documented to have the ability to change the conformation of a very important helix (helix 12, for those keeping score at home).

When estradiol binds the ER, this particular helix takes on a conformation that allows DNA transcription to mRNA, and estrogenic effects are then expressed in the body. When Nolvadex (Tamoxifen) binds to it, the antagonist changes the shape of this helix in such a way that it now folds (or bends) in such a way to prevent proper binding of estrogen, and subsequent transcription of DNA to mRNA.

The ER (remember, no George Clooney, no Anthony Edwards) contains two areas called AF-1 and AF-2. Nolvadex actually only inactivates AF-2. Since there are two areas that can can initiate transcription of mRNA, and Nolvadex is estrogenic in some tissues but an anti-estrogen (sort of) in others,it is possible that AF-1 is the dominant domain of estrogen gene transcription in the liver (for example) but not in mammary (breast) tissue. Thus, Nolvadex exerts different effects as regards estrogen, in different tissues.

Hence, we can see that the effect of Nolvadex is via the mechanism of estrogen receptor blockade of breast tissue [1]. Contrary to popular opinion, total body estradiol actually increases with use of Nolvadex. It is not, as it’s often called an “Anti-Estrogen.”


Some other positive effects of Nolvadex (acting this time as an estrogen agonist) is that it can be beneficial to a properly functioning immune system as well as your lipid profile (cholesterol) should also show marked improvement with administration of tamoxifen^[2]. It’s actually very useful stuff during a cycle for immune, joint, and lipid benefits.

Nolvadex also has some highly important and practical roles for a steroid using athlete who is coming off a cycle. Hypogonadic and infertile men given Nolvadex, saw significant increases in the serum levels of LH, FSH, as well as testosterone levels [3][4]. In fact, 20mgs of Nolvadex can possibly raise your testosterone levels approximately 150% [5]. SO clearly this is something we should consider using not only during a cycle to prevent gyno, but especially afterwards, to restore our natural hormonal function.

Unfortunately, it has been linked to reduced gains in some bodybuilders. This is as a possible result of Nolvadex’s potential to possibly reduce IGF (Insulin-like-Growth-Factor) levels, which are important for muscle growth. Additionally, some people report vision problems with its use, but I didn’t find that to be the case for me.

Still, for PCT, or even on a cycle, most people find Nolvadex to be an indispensable product.